Erlotinib得舒緩Tarceva ®
main article: Molecularly Targeted therapeutic agents MOA:Targeted therapy(MoAb和Small molecules in targeted therapy for cancer, often synthetic癌症標靶療法中的小分子,通常為合成)中的Small molecules in targeted therapy for cancer, often synthetic A reversible receptor tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR).binding to adenosine triphosphate (ATP) binding site of the receptor on receptor tyrosine kinase inhibitor. For the signal to be transmitted, two EGFR molecules need to come together to form a homodimer. These then use the molecule of ATP to trans-phosphorylate each other on tyrosine residues, which generates phosphotyrosine residues, recruiting the phosphotyrosine-binding proteins to EGFR to assemble protein complexes that transduce signal cascades to the nucleus or activate other cellular biochemical processes. When erlotinib binds to EGFR, formation of phosphotyrosine residues in EGFR is not possible and the signal cascades are not initiated. biomarker Patients who are non-smokers, and light former smokers, with adenocarcinoma or subtypes like BAC are more likely to have EGFR mutations, but mutations can occur in all types of patients. A test for the EGFR mutation in cancer patients has been developed by Genzyme. Erlotinib has recently been shown to be a potent inhibitor of JAK2V617F activity. JAK2V617F is a mutant of tyrosine kinase JAK2, is found in most patients with polycythemia vera (PV) and a substantial proportion of patients with idiopathic myelofibrosis or essential thrombocythemia. The study suggests that erlotinib may be used for treatment of JAK2V617F-positive PV and other myeloproliferative disorders. The drug's US patent will expire in 2020.http://drugpatentwatch.com/p/ingredient/erlotinib, "Details for Generic Name: erlotinib", ''DrugPatentWatch.com In May 2012, the US District Court of Delaware passed an order in favour of OSI Pharmaceutical LLC against Mylan Pharmaceuticals upholding the validity of the patent for Erlotinib. In India, generic pharmaceutical firm Cipla is battling with Roche against the Indian patent for this drug. Medical uses non-small cell lung cancer非小細胞肺癌 *The SATURN (Sequential Tarceva in Unresectable NSCLC) study found that erlotinib added to chemotherapy improved **Survival rate ***overall survival by 19%, and ***improved progression-free survival (PFS) by 29%, when compared to chemotherapy alone.2009 - SATURN: A double-blind, randomized, phase III study of maintenance erlotinib versus placebo following nonprogression with first-line platinum-based chemotherapy in patients with advanced NSCLC.April 2010 - Tarceva Indication Announcement Letter *The U.S. Food and Drug Administration (FDA) has approved erlotinib for : **the treatment of locally advanced or metastatic non-small cell lung cancer that has failed at least one prior chemotherapy regimen. In lung cancer, erlotinib has been shown to be effective in patients with or without EGFR mutations, but appears to be more effective in patients with EGFR mutations. Overall survival, progression-free survival and one-year survival are similar to standard second-line therapy (docetaxel or pemetrexed). Overall response rate is about 50% better than standard second-line chemotherapy. locally advanced, unresectable, or metastatic pancreatic cancer In November 2005, the FDA approved erlotinib in combination with gemcitabine for treatment of locally advanced, unresectable, or metastatic pancreatic cancer.Takimoto CH, Calvo E. "Principles of Oncologic Pharmacotherapy" in Pazdur R, Wagman LD, Camphausen KA, Hoskins WJ (Eds) Cancer Management: A Multidisciplinary Approach. 11 ed. 2008. 參考資料 20170924wikipedia-Erlotinib 分類:Erlotinib得舒緩Tarceva ® 分類:Targeted therapy標靶療法